Antihypertensive drugs, specific agents

The inhibition of ACE, located in different tissues (e.g., plasma, lung, kidney, heart, skeletal muscle, pancreas, brain) may influence various regulatory systems (Ondetti and Cushman, 1984). ACE plays a pivotal role in two independent humoral systems that affect blood pressure, since it is responsible for the generation of a vasopressor agent, angiotensin II, and for the inactivation of a vasodepressor agent, bradykinin. Many specific ACE-inhibitors have been developed for use as a potent, orally administered antihypertensive drug (Wyvratt and Patchett, 1985). 

While the main goal of antihypertensive therapy is to achieve target blood pressures, the selection of agents for an individual should also account for certain special considerations and a patient s comorbidities. Specific antihypertensive therapy is warranted for certain patients with comorbid conditions that may elevate their level of risk for cardiovascular disease. Clinical conditions for which there is compelling evidence supporting one or more classes of drug therapy include 2... 

The renaissance of the Biginelli MCR can be attributed to the obtained pyrimidine derivatives, which show remarkable pharmacological activity. A broad range of effects, including antiviral, antitumor, antibacterial, anti-inflammatory as well as antihypertensive activities has been ascribed to these partly reduced pyrimidine derivatives [96], such as 9-117 and 9-118 (antihypertensive agents) [97] and 9-119 (ala-adrenoceptor-selective antagonist) [98] (Scheme 9.24). Recently, the scope of this pharmacophore has been further increased by the identification of the 4-(3-hydroxyphenyl)-pyrimidin-2-thione derivative 9-120 known as monastrol [98], a novel cell-permeable lead molecule for the development of new anticancer drugs. Monastrol appears specifically to affect cell division (mitosis) by a new mechanism,... 

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